Pemoline (Oral)

As a dopaminergic, the drug resembles the structure of methylphenidate and amphetamines. The drug is a white in color, tasteless, relatively insoluble and odorless powder. The drug’s solubility in 90-94% ethyl is 2.2 mg/mL.


Pemoline is similar to amphetamine when it comes to pharmacological effects. However, it is a mild stimulant than the latter and contains lesser potent sympathomimetic properties. The drugs is also characterized by a slower onset of action and a longer half-life, i.e. (12'16 h).

Pemoline's primary use or mechanism of action is that it acts as DAT inhibition. Initially, the drug was approved for treatment of attention-deficit/hyperactivity disorder (ADHD). However, with time, the drug was discovered to have some unlikely side effects that made the authorities review its usage for the condition. The main reason the drug was withdrawn from the US market in 2005 is its relation to generic products assumed to increase the risk or cause fatal hepatotoxicity.

In the past, Pemoline has in many instances been associated with various hepatic failure. For this reason, medical experts advise that the drug should not be considered as the first line of action or drug therapy in the case of ADHD treatment. It's also imperative to consult your physician before you start the dosage so that you can undergo a medical check to ensure no underlying liver disease. The treatment is viable for people with a normal baseline liver functionality.

The physician will put you on Monitor to observe your baseline levels and do so for at least two weeks. It is advisable to stop the treatment if the serum ALT (SGPT) gets increased to a clinically acceptable level. Any increase that is greater than or equivalent to 2 times the normal upper limits or if there are signs to indicate a possible liver failure should indicate that the treatment should be terminated immediately. Also, before commencing the treatment, patients are asked to fill written informed consent and submit it together with your patient files.

Conditions Treated

  • Attention-deficit hyperactivity disorder (ADHD)
  • Narcolepsy

Type Of Medicine

  • Dopaminergic

Side Effects

Apart from being removed by the FDA, there are various documented side effects of the drug. Being a nervous system stimulant, it goes without saying that the drug must contain some adverse side effects on the user. Below are some adverse reactions as arranged in descending order of severity as contained in each category that is associated with the drug.

Hepatic: As mentioned earlier, one of the reasons that the drug got withdrawn by the FDA as a treatment for ADHD was its implication to hepatic failure. Numerous reports on hepatic dysfunction as a result of the drug have been documented, ranging from asymptomatic increases in the liver enzymes to possible hepatitis. In extreme cases, the drug causes jaundice and in fewer cases lead to hepatic failure. It is advisable for patients taking CYLERT to view the precautions and warning segment on the drug to ascertain its effects.

Central Nervous System: Being a nervous system stimulant, the most adverse side effects are felt on the same. Among the reported side effects on the nervous system includes convulsive seizures. Although not scientifically proven, further literature asserts that Pemoline is responsible for various cases of the Gilles de la Tourette syndrome attack or onset. Other side effects include hallucinations; dyskinetic tongue, lips, and face movements. The drug also causes abnormal oculomotor function that includes oculogyric crisis and nystagmus; dizziness; a headache; mild depression; drowsiness; and increased irritability.

One of the frequently documented side effects of Pemoline has to be Insomnia. For many patients, the effect usually starts occurring in the very first sessions of therapy. In the majority of reported cases, the insomnia is transient, or in other words, it responds effectively to a certain reduction in the dosage.

Gastrointestinal: there have also been reports that Anorexia or extreme weight loss could possibly occur in the first few weeks of therapy. However, a majority of the reported cases indicate that, just like insomnia, anorexia is also transient. Patients should expect to gain weight around three months into the treatment regimen. Also, in rare cases, patients have reported experiencing stomach aches and nausea.

Miscellaneous: in rare cases, patients have reported that the drug causes suppressed growth in babies over a long period of time. The drug also causes skin rashes in children.
While many side effects could be an indication of a serious underlying problem, there are effects that if they occur you should see a physician immediately. They include;

  • Yellow eyes
  • Dark urine
  • Shortness of breath, troubled breathing, wheezing, or tightness in chest
  • Convulsions (seizures)
  • Nausea and vomiting
  • Hallucinations (seeing, hearing, or feeling things that are not there)
  • Unusual bleeding or bruising
  • Skin rash
  • Unusual tiredness
  • Swollen or painful glands
  • Sweating and restlessness and vomiting

There are also some various side effects of the drug may occur which do not need you to see a physician. These side effects fizzle away on their own. However, if you feel bothered by them, you could consult your physician for answers. They include;

  • Appetite loss
  • Insomnia

The rare effects:

  • Increased irritability
  • Dizziness
  • Mental depression
  • Drowsiness
  • Stomachache


On how to take the drug, many times its advisable to consult with your physician on the way forward. Different dosages depend on different patient conditions, and your physician will be able to determine which dosage is suitable for you. Normally, Pemoline (CYLERT) is administered every morning in a single dose.

The general recommended dosage is 37.5 mg/day which then increases to 18.75 mg in one-week intervals till the dose is finished or achievement of the anticipated clinical outcome. For a majority of patients, the most effective dose ranges from 56.25 to 75 mg with the maximum dose being pemoline is 112.5 mg daily.
It's imperative to note that the desired clinical outcomes with CYLERT are not instant but gradual. If you follow the recommended dosage titration, you may not experience significant benefits until the fourth week of using the drug. If possible, it is advisable that medication is interrupted once in a while to determine any recurrence of any behavioral symptoms under treatment. This will help determine if to continue or terminate therapy.

Also, remember that different conditions call for different dosages. Do not share the Pemoline drug with anyone even if you have the same medical condition. The Pemoline dosage will in many instances be different for different patients. You must follow your physician's orders or the given directions on the label. While the above information on the label may be the same, if you find that your dose is different do not change it unless instructed by the doctor.

For Children under in the 6 years and over the bracket, you should start at 37.5 milligrams (mg) daily in the morning. If the condition being treated is severe, the doctor may feel the need to increase the dosage. However, the dosage will never go above 112.5 mg a day. For children below six years of age, the dosage should strictly be directed by the doctor.

Drug Interactions

Before you embark on pemoline drug therapy, it's imperative to tell your doctor about any underlying issues that you have that could interfere with the drug. Before you take the drug, your doctor needs t weigh between the good and bad of the drug for you. You need to state any drugs that you are using so that the doctor can assess if the drug can safely interact with pemoline.

You need to let your doctor know if you have any allergies caused by other drugs. Generally, you should state all the allergies you have and the drugs you're taking for that allergy. This will make it easier to determine how Pemoline interacts with the drugs.

Due to its lethal effects, CYLERT has not been adversely researched on humans. For that CYLERT's interaction of with other drugs has faced obstacles when it comes to human studies. However, there are known cases where patients taking Pemoline with any other drugs especially the ones that have CNS activity need to notify their physicians to increase monitoring. There have also been reports of reduced seizure threshold in patients taking CYLERT combined with other antiepileptic medications.

In many cases, the interaction of Pemoline with other drugs results in different reactions on the body, and so consultations are essential. While there hasn't been a lot of research on the interaction of the drug with other drugs, there are close to 405 drugs known to interact with Pemoline. Some of the drugs include:

  • Acetaminophen / tramadol
  • Adcetris (brentuximab)
  • B-Donna Tablets (atropine / hyoscyamine / phenobarbital / scopolamine)
  • Barbidonna (atropine / hyoscyamine / phenobarbital / scopolamine)
  • Carbamazepine
  • Carbatrol (carbamazepine)


Due to its implications on life-threatening Liver failure, Pemoline should not be used as a first choice drug for ADHD. Since its first marketing in the year 1975, there have been 13 reported instances of acute liver failure filed to the FDA. While the approximated number of filed cases is not significantly large enough to be considered an epidemic, the reporting rate ranges from four to seventeen times the expected range of the general population.

These estimates may turn out inaccurate because not every case is reported. Also, the fact that the length between the onset of the drug use and the resulting hepatic failure is long and so recognition may be limited. This means the association between the hepatic failure and pemoline may not be as accurate. Supposed a portion of the actual cases got reported on a daily basis, then the risk would be classified as being significantly higher.

Among the 13 reported cases in the late 90s, before the drug was withdrawn later in 2005, eleven of the cases led to death while the others got a liver transplant. The transplant is only effective within the first 4 weeks when the signs of possible liver failure are diagnosed.
Although various reports have described the drug as causing dark urine, other studies have shown symptoms like; anorexia, gastrointestinal symptoms and malaise (prodromal symptoms). Pemoline use should be terminated immediately if the physician observes a clinically hepatic dysfunction in the course of its usage.

For children, there has been numerous reports of decreased growth in height and weight as a result of the drug use. Long-term usage of the stimulant on children has been attributed to delayed growth in children and younger teens. It is therefore imperative that for long-term usage you ensure close monitoring by your physician.


Like many other drugs, you should store the drug in a closed container. This ensures no moisture gets into the container. The drug should be kept away from direct sunlight and should be stored under room temperature. You should keep it away from heat and freezing. Also, keep out of reach of children. It is also essential that you do not keep any outdated medicine in the house.


Pemoline is a chewable drug administered orally. It's among the group of drugs known as central nervous system (CNS) stimulants. The drug is mainly used to treat children and your teenagers with (ADHD) attention deficit hyperactivity disorder.

The drug works by increasing the attention span of the children and decreasing restlessness in overactive children. Pemoline is overly effective in children that cannot concentrate for too long or children that are emotionally unstable. However, the drug's implication to causing delayed growth in children has led to its decreased popularity as a preferred drug for children.

While it happens rarely, Pemoline has been attributed to causing liver problems. It is then advisable that patients speak to their doctors about the treatment before starting the therapy. The doctor takes you through the basics of the drug then asks you to sign an informed consent form to indicate that you understand everything stated about the drug. This is imperative to ensure you understand that the drug could cause complications like liver problems. While Pemoline is one of the best drugs for ADHD, it is only available with a doctor's prescription.